Abstract
Soursop leaf chloroform extract has anticancer activity. The active ingredient of soursop leaf was acetogenin polypoid derivatives that have a lipophilic characteristic, and less effective to achieve action targets of drugs in biological systems. The Self-Micro Emulsifying Drug Delivery System (SMEDDS) was an effective drug delivery technique that increases the solubility of lipophilic drugs. This study aims to determine the proportion of optimum SMEDDS formula using Simplex Lattice Design (SLD) method. The Formula of SMEDDS was prepared using a combination of Tween 80-Croduret, Propylene Glycol, and Candlenut oil. Optimization formula with SLD method using Design-Expert software based on physical stability parameters there are the percent of transmittance and emulsification time. The optimum formula of SMEDDS was compared with SLD prediction formula using a statistical analysis t-test, then test of loading dose extract, stability test accelerated by centrifugation, particle size, and zeta potential. The proportion of optimum composition of Tween 80-Croduret, Propylene Glycol, and Candlenut oil of SMEDDS was 60.87%; 24.13%; 15.00% respectively. Results of transmittance 41.14±3.78% and emulsification time 119.0±2.08 seconds. The predicted SLD value for the transmittance percent was 55.0% and the emulsification time was 119.59 seconds. The result of the statistical analysis of one sample t-test showed no significant difference between observation results and SLD prediction. The SMEDDS system has F value of 0.99 and capable to load 25.0 mg chloroform extract of soursop leaf each system with an average particle size of 440 nm and zeta potential of +21.5 mV.
Highlights
The natural ingredients of active compounds of extract for medical treatment were considered safer than synthetic drugs because it was easy to obtain, has low side effects, did not cause interaction and dependence (Lynch and Berry, 2007)
Chloroform solvent was chosen because according to the research of Astirin et al, (2013) that the soursop leaf fraction in chloroform solvent resulted in a higher percentage of apoptosis compared with ethyl acetate solvent in MTT test of Hela cancer cell
Polydispersity index showed a low value of particle size distribution, it was mean that the particle size in Selfmicroemulsifying drug delivery system (SMEDDS) was uniform (Avachat and Patel, 2014)
Summary
The natural ingredients of active compounds of extract for medical treatment were considered safer than synthetic drugs because it was easy to obtain, has low side effects, did not cause interaction and dependence (Lynch and Berry, 2007). Paulinus et al, (2013), suggests that Annona muricata ethanol extract at a dose of 100 mg/kg body weight has protective activity against rat’s. Formulation technology to improve the bioavailability of drugs that were less soluble in water by using inclusion technique, which was the delivery of lipid-based drugs (Kuentz, 2011). Microemulsions had a particle size range of 100500 nm (Khan et al, 2011), small size makes the surface area of the absorption larger, so increasing the solubility of lipophilic compounds in water as well as increasing the bioavailability of orally administered drugs (Wang et al 2014). SMEDDS will form an oil in water emulsion [o/w] in the gastrointestinal tract spontaneously, the presence of surfactant will alter the permeability and increase the solubility of the drug, and protect from hydrolysis by enzymes, increasing drug
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